作者：Huaihong Zhang,Zhaosheng Cai,Yu Sun,Fei Yu,Yaoqiang Chen,Baiwang Sun*
关键字：folate, cyclodextrins, click chemistry, tumor targeted
论文来源：期刊
发表时间：2012年
To enhance site-speci?c intracellular delivery against the folate receptor, a drug carrier was designed and synthesized by bioconjugation of folic acid (FA) to b-cyclo-dextrins (b-CD) through a poly(ethylene glycol) (PEG) spacer from ‘‘click chemistry’’ strategy. The resulted conjugates were con?rmed by 1H NMR and IR spectroscopy. Host–guest interactions between hydrophobic drug and b-CD are capable of entrapping a hydrophobic drug, like 5-Fluorouracil, to form drug-b-CD-PEG-FA nanoparticles (NPs) in aqueous solution. The morphology and size of b-CD-PEG-FA NPs were measured by transmission electron microscopy (TEM) and dynamic light scattering (DLS). The targeting ability of the b-CD-PEG-FA NPs was investigated against two kinds of cell lines (HeLa and A549), which have different amounts of folate receptors on their surface. Confocal image analysis revealed that b-CD-PEG-FA conjugate-assembled nanoparticles exhibited a greater extent of cellular uptake against HeLa cells than A549 cells. This suggests folate-receptor-mediated endo-cytosis can affect the cellular uptake ef?ciency of drug-loaded b-CD-PEG-FA NPs. The b-CD-PEG-FA conjugates that are presented may be promising active tumor-targeting carrier candidates via folate mediation.